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Assay Detail

CHEMBL888517

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonist activity at human P2Y1 receptor expressed in 1321N1 cells assessed as inhibition of 2-MeS-ADP-induced inositol phosphate formation
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type 1321-N1
Confidence 9 — Direct single protein target
Curated By Expert

Target

P2Y purinoceptor 1 (CHEMBL4315)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

P2Y1 antagonists: combining receptor-based modeling and QSAR for a quantitative prediction of the biological activity based on consensus scoring.
Costanzi S, Tikhonova IG, Ohno M, Roh EJ, Joshi BV, Colson AO, Houston D, Maddileti S, Harden TK, Jacobson KA.
J Med Chem (2007) 50 : 3229 -3241
PubMed 17564423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.98 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390149 1 7.03
CHEMBL153254 1 6.21
CHEMBL227235 1 6.10
CHEMBL226857 1 6.06
CHEMBL375022 1 5.81
CHEMBL226807 1 5.76
CHEMBL435930 1 5.71
CHEMBL375682 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390149 IC50 = 93.0 nM 7.03
CHEMBL153254 IC50 = 620.0 nM 6.21
CHEMBL227235 IC50 = 790.0 nM 6.10
CHEMBL226857 IC50 = 870.0 nM 6.06
CHEMBL375022 IC50 = 1560.0 nM 5.81
CHEMBL226807 IC50 = 1750.0 nM 5.76
CHEMBL435930 IC50 = 1940.0 nM 5.71
CHEMBL375682 IC50 = 6900.0 nM 5.16